摘要:
This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译:本发明提供具有以下结构的式1的孕酮受体拮抗剂,其中T为O,S或不存在; R 1,R 2和R 2各自独立地为氢,烷基,取代的烷基; 或R 1和R 2一起形成环,并且一起含有-CH 2(CH 2)2 CH 2 CH 2 - , - CH 2 CH 2 CH 2 CH 2 N 2 CH 2 2 CH 2 - , - O(CH 2)2 CH 2 - , - (CH 2 CH 2) O(CH 2 CH 2)q O - , - CH 2 CH 2 OCH 2 - / SUB CH 2,或CH 2 CH 2,NR 7,CH 2,CH 2, CH 2 - ; n = 1-5; p = 1-4; q = 1-4; R 3是氢,OH,NH 2,烷基,取代的烷基,烯基,取代的烯基,炔基,取代的炔基或COR A。 R A是氢,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R 4是氢,卤素,CN,NH 2,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R 5是氢,烷基或取代的烷基; R 6是氢,烷基,取代的烷基或COR B; R B是氢,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R 7是氢或烷基; 或其药学上可接受的盐。
摘要:
Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.
摘要:
This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
摘要:
This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.
摘要翻译:本发明涉及作为孕酮受体拮抗剂的取代二氢吲哚衍生物化合物,其制备方法和药物应用,特别是包括具有以下一般结构的良性或恶性肿瘤疾病的避孕和治疗:其中R 1和 R 2可以是单个取代基或稠合形成螺环。
摘要:
This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要:
This invention relates to methods of co-administering compounds of formula 1 which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, with estrogen, an estrone, or an estrogen receptor agonist for contraception, hormone replacement therapy, or treating progesterone-related carcinomas and adenocarcinomas.
摘要翻译:本发明涉及共同施用式1化合物的方法,其为具有以下通式结构的孕酮受体的激动剂:其中:R 1,R 2,R 2, R 3,R 4,R 5和Q 1如本文所定义,或其药学上可接受的盐,与 雌激素,雌激素或雌激素受体激动剂用于避孕,激素替代治疗或治疗孕激素相关的癌和腺癌。
摘要:
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要:
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要:
The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.
摘要:
Non-steroidal tricyclic quinolinone and tricyclic quinoline compounds and compositions that are agonists, partial agonists and/or antagonists for androgen receptors (AR), their preparation and their uses are described.